Design, synthesis, and biological evaluation of chalcone-linked thiazole-imidazopyridine derivatives as anticancer agents

Suma, V. Ragha; Sreenivasulu, Reddymasu; Rao, Mandava V. Basaveswara; Subramanyam, M.; Ahsan, Mohamed Jawed; Alluri, Ramesh; Rao, K. Ram Mohan

doi:10.1007/s00044-020-02590-9

Cited by 45 publications

(22 citation statements)

References 61 publications

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“…Encouraged by the data from the literature regarding the anticancer activity of chalcones [132][133][134][135][136], Suma et al [137] designed and synthesized a library of chalcone-linked thiazole-imidazopyridine (87a-j, Figure 34) with the purpose to study their anticancer activity. Compounds were tested on the following four human cancer cell lines MCF-7 (breast carcinoma), A549 (lung carcinoma), DU-145 (prostate carcinoma), and MDA MB- The presence of the bromine and methoxy group was more beneficial for O-noscapine derivatives 86o and 86c compared to N-noscapinoids (86o, 86c).…”

Section: Thiazole Derivatives As Anticancer Agentsmentioning

confidence: 99%

Thiazole Ring—A Biologically Active Scaffold

2021

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Background: Thiazole is a good pharmacophore nucleus due to its various pharmaceutical applications. Its derivatives have a wide range of biological activities such as antioxidant, analgesic, and antimicrobial including antibacterial, antifungal, antimalarial, anticancer, antiallergic, antihypertensive, anti-inflammatory, and antipsychotic. Indeed, the thiazole scaffold is contained in more than 18 FDA-approved drugs as well as in numerous experimental drugs. Objective: To summarize recent literature on the biological activities of thiazole ring-containing compounds Methods: A literature survey regarding the topics from the year 2015 up to now was carried out. Older publications were not included, since they were previously analyzed in available peer reviews. Results: Nearly 124 research articles were found, critically analyzed, and arranged regarding the synthesis and biological activities of thiazoles derivatives in the last 5 years.

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Section: Thiazole Derivatives As Anticancer Agentsmentioning

confidence: 99%

Thiazole Ring—A Biologically Active Scaffold

2021

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“…Recently, studies have illustrated that N-heterocyclic compounds possess antiviral activity. Thus, they can be used as potential noncovalent inhibitors of 3CL pro of SARS-CoV-2. − Some of the most prominent nitrogen-containing heterocycles are the purine scaffolds, which have attracted medicinal interest due to their applications as drug candidates in cancer treatment and viral disorders. , Also, there is a considerable tendency to study new heterocyclic fused imidazopyridine derivatives containing abundant biological activities, such as anticancer, , antiprotozoal agent, antiviral, anti-inflammatory, and anti-Alzheimer’s disease activities. Recent investigations have revealed that the heterocyclic systems with additional fused rings display more effective pharmacological and physicochemical properties.…”

Section: Introductionmentioning

confidence: 99%

Pyrido[1,2-e]purine: Design and Synthesis of Appropriate Inhibitory Candidates against the Main Protease of COVID-19

et al. 2022

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A series of tricyclic and polycyclic pyrido[1,2- e ]purine derivatives were designed and synthesized via a two-step, one-pot reaction of 2,4-dichloro-5-amino-6-methylpyrimidine with pyridine under reflux conditions. Various derivatives of pyrido[1,2- e ]purine were also synthesized by substituting the chlorine atom with secondary amines. After careful physiochemical and pharmacokinetic predictions, the inhibitory effects of the synthesized compounds against the main protease of SARS-CoV-2 have been evaluated by molecular docking and molecular dynamics approaches. The in silico results revealed that among all of the studied compounds, the morpholine/piperidine-substituted pyrido[1,2- e ]purine derivatives are the best candidates as effective inhibitors of SARS-CoV-2.

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“…Docking studies were performed on three potential targets: protein kinases CLK1 (5X81), EGFR (2J5F), and tubulin (1SAO). Scores obtained indicated a correlation between the activity of compounds and their action on CLK1 [ 239 ].…”

Section: Synthetic Derivatives Of Chalcones With Anticancer Propertiesmentioning

confidence: 99%

Anticancer Activity of Natural and Synthetic Chalcones

Constantinescu

Lungu²

2021

IJMS

103

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Cancer is a condition caused by many mechanisms (genetic, immune, oxidation, and inflammatory). Anticancer therapy aims to destroy or stop the growth of cancer cells. Resistance to treatment is theleading cause of the inefficiency of current standard therapies. Targeted therapies are the most effective due to the low number of side effects and low resistance. Among the small molecule natural compounds, flavonoids are of particular interest for theidentification of new anticancer agents. Chalcones are precursors to all flavonoids and have many biological activities. The anticancer activity of chalcones is due to the ability of these compounds to act on many targets. Natural chalcones, such as licochalcones, xanthohumol (XN), panduretin (PA), and loncocarpine, have been extensively studied and modulated. Modification of the basic structure of chalcones in order to obtain compounds with superior cytotoxic properties has been performed by modulating the aromatic residues, replacing aromatic residues with heterocycles, and obtaining hybrid molecules. A huge number of chalcone derivatives with residues such as diaryl ether, sulfonamide, and amine have been obtained, their presence being favorable for anticancer activity. Modification of the amino group in the structure of aminochalconesis always favorable for antitumor activity. This is why hybrid molecules of chalcones with different nitrogen hetercycles in the molecule have been obtained. From these, azoles (imidazole, oxazoles, tetrazoles, thiazoles, 1,2,3-triazoles, and 1,2,4-triazoles) are of particular importance for the identification of new anticancer agents.

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Design, synthesis, and biological evaluation of chalcone-linked thiazole-imidazopyridine derivatives as anticancer agents

Cited by 45 publications

References 61 publications

Thiazole Ring—A Biologically Active Scaffold

Thiazole Ring—A Biologically Active Scaffold

Pyrido[1,2-e]purine: Design and Synthesis of Appropriate Inhibitory Candidates against the Main Protease of COVID-19

Anticancer Activity of Natural and Synthetic Chalcones

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